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    • 1. 发明授权
    • Processes for preparing aminophenylsulfonylureas, and intermediates therefor
    • 制备氨基苯磺酰脲的方法及其中间体
    • US06500952B1
    • 2002-12-31
    • US09664201
    • 2000-09-18
    • Gerhard SchnabelJan VermehrenLothar Willms
    • Gerhard SchnabelJan VermehrenLothar Willms
    • C07D23942
    • C07D521/00A01N47/36H01R33/06Y02A40/143
    • The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R21, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)—Het, where Ar=phenyl, M=H or cation and Het=heterocycle from formula (I), to give compounds (I) (A=H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A=H), or c) reaction of (III) with cyanates and amines (VIII) of the formula HNR3—Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A=H) and optional acylation if A is to be other than H. Compounds of the formulae (I) (A=H), (III), (IV), (V), (VI) (M=cation) and (VII) are novel.
    • 本发明涉及化合物(Ⅰ)的制备,其中A = H或酰基,R 1,R 21,R 3,R 4,n,X,Y和Z如权利要求1中所定义,通过卤化和重排化合物 任选的盐),得到化合物(III)a)(III)至(IV)的氨解,硝基的还原和与式Ar-OCO-N(M)-Het的氨基甲酸酯(盐)(VI)的反应, 其中Ar =苯基,M = H或阳离子和Het =来自式(I)的杂环,得到(III)至(IV)化合物(I)(A = H),orb)氨解,与氨基甲酸酯 (VI)和还原所得化合物(VII)在NO 2基团上得到化合物(I)(A = H),orc)(III)与式HNR3-Het的氰酸酯和胺(VIII)的反应,还原 所得到的化合物(Ⅶ)在NO2基团上得到化合物(I)(A = H),任选的酰化如果A不为H.式(I)(A = H),(III) (IV),(V),(VI)(M =阳离子)和(VII)是新颖的。
    • 2. 发明授权
    • Processes for the preparation of aminophenylsulfonyl-ureas and intermediate products for the processes
    • 用于制备氨基苯磺酰脲和中间产物的方法
    • US06790955B2
    • 2004-09-14
    • US10288052
    • 2002-11-05
    • Gerhard SchnabelJan VermehrenLothar Willms
    • Gerhard SchnabelJan VermehrenLothar Willms
    • C07D27300
    • C07D521/00A01N47/36H01R33/06Y02A40/143
    • The invention relates to the preparation of compounds (I) in which A═H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)-Het, where Ar=phenyl, M═H or cation and Het=heterocycle from formula (I), to give compounds (I) (A═H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A═H), or c) reaction of (III) with cyanates and amines (VII) of the formula HNR3-Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A═H) and optional acylation if A is to be other than H. Compounds of the formulae (I) (A═H), (III), (IV), (V), (VI) (M=cation) and (VII) are novel.
    • 本发明涉及其中A = H或酰基和R 1,R 2,R 3,R 3,n,X,Y和Z如权利要求1中所定义的化合物(I)的制备, 化合物(II)(任选盐)的卤化和重排以得到化合物(III)a)(III)至(IV)的氨解,还原硝基并与式Ar-的氨基甲酸酯(盐)(Ⅵ) 其中Ar =苯基,M = H或阳离子和Het =来自式(I)的杂环,得到化合物(I)(A = H),orb)氨解(III)至(III) IV),与氨基甲酸酯(盐)(VI)的反应和NO 2基团上得到的化合物(VII)的还原,得到化合物(I)(A = H),orc)(III)与氰酸酯和胺的反应(VII) 的式(HNR 3)-Het,并且在NO 2基上还原所得化合物(Ⅶ),得到化合物(I)(A = H),并且如果A不为H,则为任意的酰化。式 I)(A = H),(III),(IV),(V),(VI)(M =阳离子)和(VII)
    • 4. 发明申请
    • Processes for preparing aminophenylsulfonylureas, and intermediates therefor
    • 制备氨基苯磺酰脲的方法及其中间体
    • US20050033047A1
    • 2005-02-10
    • US10936180
    • 2004-09-08
    • Gerhard SchnabelJan VermehrenLothar Willms
    • Gerhard SchnabelJan VermehrenLothar Willms
    • C07D251/16A01N47/36A01P13/00A01P21/00C07C309/89C07C311/39C07D239/42C07D239/46C07D239/47C07D239/52C07D251/42C07D251/44C07D251/46C07D521/00F21S4/00F21V31/00H01R33/06A01N43/54A01N43/90C07D239/02
    • C07D521/00A01N47/36H01R33/06Y02A40/143
    • The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III)  R*═OH, R**═NR1R2  (II) R*═NR1R2, R**═Cl  (III) R*═NR1R2, R**═NH2  (IV) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)-Het, where Ar=phenyl, M=H or cation and Het=heterocycle from formula (I), to give compounds (I) (A=H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A=H), or c) reaction of (III) with cyanates and amines (V) of the formula HNR3−Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A=H) and optional acylation if A is to be other than H. Compounds of the formulae (I) (A=H), (III), (IV), (V), (VI) (M=cation) and (VII) are novel.
    • 本发明涉及其中A = H或酰基和R 1,R 2,R 3,R 3,n,X,Y和Z如权利要求1中所定义的化合物(I)的制备, 化合物(II)(任选盐)的卤化和重排,得到化合物(III)R * = OH,R ** = NR 1 R 2(II)R * = NR 1 R 2, R ** = Cl(III)R * = NR 1 R 2,R ** = NH 2(IV)a)(III)至(IV)的氨解,硝基还原和与氨基甲酸酯反应 其中Ar =苯基,M = H或阳离子和Het =来自式(I)的杂环的式Ar-OCO-N(M)-Het的化合物(I)(A = H) ,或b)(III)至(IV)的氨解,与氨基甲酸酯(盐)(VI)的反应和所得化合物(VII)在NO 2基团上的还原,得到化合物(I)(A = H),或c) (III)与式HNR <3-> Het的氰酸酯和胺(V)的反应,并且在NO 2基团上还原所得化合物(VII),得到化合物(I)(A = H),任选的酰化如果A 式(I)(A = H),(III),(IV),(V),(VI)(M = on)和(VII)是新颖的。
    • 6. 发明授权
    • Method of controlling undesired plant growth in rice
    • 控制水稻不希望的植物生长的方法
    • US6017852A
    • 2000-01-25
    • US77139
    • 1998-05-21
    • Gerhard SchnabelLothar WillmsKlaus Bauer
    • Gerhard SchnabelLothar WillmsKlaus Bauer
    • C07D251/46A01N47/36C07D239/52C07D521/00A01N43/54A01N43/66
    • C07D521/00A01N47/36
    • The invention relates to a method of controlling harmful plants in rice crops, which comprises applying one or more compounds of the formula (I) or salts thereof whereR.sup.1 is an acyl radical from the group CO--R.sup.2, CS--R.sup.2, CO--OR.sup.3, CS--OR.sup.3, CO--SR.sup.4, CS--SR.sup.4, CO--NR.sup.5 R.sup.6 and CS--NR.sup.5 R.sup.6, and R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 and also X, Y and Z are as defined in the formula (I) of claim 1,to the area under cultivation, which contains the harmful plants and rice plants or their seeds, in an effective amount of from 0.0001 to 0.5 kg of a.i./ha.The compounds (I) are known per se. The invention also provides novel salts of the compounds (I).
    • PCT No.PCT / EP96 / 04798 Sec。 371日期1998年5月21日 102(e)日期1998年5月21日PCT提交1996年11月4日PCT公布。 出版物WO97 / 18711 日期:1997年5月29日本发明涉及一种控制水稻作物中有害植物的方法,其包括应用一种或多种式(I)化合物或其盐,其中R 1为酰基,从CO-R 2,CS-R 2 ,CO-OR3,CS-OR3,CO-SR4,CS-SR4,CO-NR5R6和CS-NR5R6以及R2,R3,R4,R5和R6,X,Y和Z如式 ),其含有有害植物和水稻植物或其种子的耕作区域的有效量为0.0001至0.5kg的ai / ha。 化合物(I)本身是已知的。 本发明还提供了化合物(I)的新型盐。
    • 9. 发明授权
    • Formylaminophenylsulfonylureas, preparation processes and use as
herbicides and plant growth regulators
    • 甲酰氨基苯基磺酰脲,制备方法和用作除草剂和植物生长调节剂
    • US5747421A
    • 1998-05-05
    • US453978
    • 1995-05-30
    • Gerhard SchnabelLothar WillmsKlaus BauerHermann BieringerChristopher Rosinger
    • Gerhard SchnabelLothar WillmsKlaus BauerHermann BieringerChristopher Rosinger
    • C07D251/16A01N47/36C07D239/42C07D251/46C07D251/50C07D405/12C07D521/00C07D239/69A01N43/54
    • C07D521/00A01N47/36
    • Formylaminophenylsulfonylureas; processes for their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) ##STR1## in which R.sup.1 is H, a substituted or unsubstituted hydrocarbon radical or an unsubstituted or substituted heterocyclic radical, R.sup.2 is H, (C.sub.1 -C.sub.6)-alkyl or (C.sub.1 -C.sub.6)-alkoxy, R.sup.3 is halogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxy, (C.sub.1 -C.sub.6)-haloalkyl, (C.sub.1 -C.sub.6)-haloalkoxy, NO.sub.2, CN, NH.sub.2, (C.sub.1 -C.sub.4) -mono- or dialkylamino, each independently of other radicals R.sup.3 if n is 2 or 3, n is 0, 1, 2 or 3, W is an oxygen atom or a sulfur atom, X and Y independently of one another are halogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxy or (C.sub.1 -C.sub.6)-alkylthio, each of the three last-mentioned radicals being unsubstituted or substituted by one or more radicals selected from the group consisting of halogen, (C.sub.1 -C.sub.4)-alkoxy and (C.sub.1 -C.sub.4)-alkylthio, or are (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.2 -C.sub.6)-alkynyl, (C.sub.2 -C.sub.6)-alkenyloxy, (C.sub.2 -C.sub.6)-alkynyloxy, mono- or di�(C.sub.1 -C.sub.4 -alkyl)!amino, and Z is CH or N, are suitable as herbicides and plant growth regulators. The compounds (I) can be prepared by processes analogous to known processes whereby some novel intermediates of formula (II) are used.
    • 甲酰氨基苯基磺酰脲 其制备方法及其作为除草剂和植物生长调节剂的用途式(I)取代烃基或未取代或取代的杂环基的化合物,R2是H,(C1-C6) - 烷基或(C1-C6) - 烷氧基,R 3为卤素,(C 1 -C 6) - 烷基,(C 1 -C 6) - 烷氧基,(C 1 -C 6) - 卤代烷基,(C 1 -C 6) - 卤代烷氧基,NO 2,CN,NH 2,(C 1 -C 4) 单或二烷基氨基,如果n为2或3,各自独立地为其它基团,n为0,1,2或3,W为氧原子或硫原子,X和Y彼此独立地为卤素,(C1 (C 1 -C 6) - 烷基,(C 1 -C 6) - 烷氧基或(C 1 -C 6) - 烷硫基,三个最后提到的基团中的每一个是未取代的或被一个或多个选自卤素,(C1- 或(C 1 -C 6) - 烷硫基,或者是(C 3 -C 6) - 环烷基,(C 2 -C 6) - 烯基,(C 2 -C 6) - 炔基,(C 2 -C 6) - 炔基氧基,(C 2 -C 6) C6) - 炔氧基,单或二[(C1-C4烷基)]氨基,Z为CH或N,适合作为除草剂和植物生长调节剂。 化合物(I)可以通过类似于已知方法的方法制备,由此使用一些新的式(II)中间体。